Omilock Capsule

Omilock Capsule

omeprazole

Manufacturer:

SM Pharmaceuticals

Distributor:

SM Pharmaceuticals
Full Prescribing Info
Contents
Omeprazole.
Description
Each capsule contains: Omeprazole 20 mg.
Action
Pharmacology: Pharmacodynamics: Mode or Mechanism of Action: Omeprazole is activated at an acidic pH to a sulphenamide derivative that binds irreversibly to H+, K+-ATPase, an enzyme system found at the secretory surface of parietal cells. It thereby inhibits the final transport of hydrogen ions (via exchange with potassium ions) into the gastric lumen. Since the H+, K+-ATPase enzyme system is regarded as the acid (proton) pump of the gastric mucosa, omeprazole is known as a gastric acid pump inhibitor. Omeprazole inhibits both basal and stimulated acid secretion irrespective of the stimulus.
Omeprazole has cytoprotective effects in rats, protecting the gastric mucosa from the effects of gastric irritants. This protective effect does not seem to be prostaglandin mediated.
Pharmacokinetics: Absorption: Rapid; 50 - 65%.
Distribution: Distributed in tissue, particularly gastric parietal cells.
Protein binding: Very high, approximately 95% bound to albumin and alpha1-acid glycoprotein.
Biotransformation: Hepatic, extensive.
Half-life: Plasma: Normal hepatic function - 30 minutes to 1 hour.
Chronic hepatic disease - 3 hours.
Onset of action: Within one hour.
Time to peak concentration: Within 30 minutes to 3.5 hours.
Time to peak effect: Within 2 hours.
Duration of action: Up to 72 hours or more (96 hours required for full restoration of acid production).
Elimination: Renal - 72 to 80%.
Fecal - 18 to 23%.
ln dialysis - Not readily dialyzable, because of extensive protein binding.
Pharmacogenetics: Pharmacokinetic studies in Asian subjects receiving single 20-mg doses of omeprazole showed an approximately fourfold increase in the area under the plasma concentration-time curve (AUC) as compared to Caucasian subjects.
Dosage adjustments should be considered for Asian patients, especially for prophylaxis of recurrence of erosive esophagitis.
Indications/Uses
Treatment of duodenal and benign gastric ulcers including those complicating NSAID therapy.
Helicobacter pylori associated peptic ulcer.
Treatment of reflux oesophagitis.
Zollinger-Ellison syndrome.
Long term therapy for patients with a history of recurrent duodenal ulcer.
Dosage/Direction for Use
Omilock Capsules are recommended to be given in the morning and swallowed whole with liquid.
For patients with swallowing difficulties the capsule might be opened and the contents swallowed or suspended in a slightly acidic fluid e.g juice, soured milk, or non-carbonated water. The dispersion should be taken immediately or within 30 minutes. Alternatively patients can suck the capsule and swallow the pellets with liquid. The pellets must not be chewed or crushed.
For duodenal and benign gastric ulcers, the usual dose is 20 mg Omilock once daily. Symptom resolution is rapid. The majority of patients with duodenal ulcer are healed after 4 weeks. The majority of patients with benign gastric ulcer are healed after 8 weeks. In severe cases, the dose may be increased to 40 mg Omilock once daily and healing is usually achieved within 4 weeks.
Long term therapy for patients with a history of recurrent duodenal ulcer is recommended at a dosage of 20 mg Omilock once daily, up to one year.
For the prevention of relapse in patients with duodenal ulcer disease, the recommended dose is Omilock 10 mg once daily. If needed, the dose can be increased to Omilock 20-40 mg daily.
Reflux oesophagitis: The recommended dosage is Omilock 20 mg once daily. Symptom resolution is rapid and in most patients healing occurs within 4 weeks. For those patients who may not be fully healed after the initial course, healing usually occurs during a further 4 weeks treatment period.
In patients with severe reflux oesophagitis, Omilock 40 mg once daily is recommended and healing is usually achieved within 8 weeks.
For the long term management of patients with healed reflux oesophagitis, the recommended dose is Omilock 10 mg once daily. If needed the dose can be increased to Omilock 20-40 mg once daily.
Zollinger-Ellison syndrome: The initial recommended dosage for patients with the Zollinger-Ellison syndrome is 60 mg once daily, but doses in the range 20 to 120 mg (three times) daily may be used; doses above 80 mg should be divided and given twice daily. In such patients treatment with omeprazole is continued as required to keep the condition under control. Zollinger- Ellison syndrome has been treated continuously with omeprazole for more than 5 years.
Helicobacter pylori-associated peptic ulcer disease: The usual dose is omeprazole capsule 40 mg daily with oral amoxycillin 1.5 g daily (given as 750 mg twice daily) for 2 weeks. In clinical studies, daily dose of 1.5 to 2 g of amoxycillin have been used.
Impaired renal function: Dose adjustment is not required in patients with impaired renal function.
Impaired hepatic function: As bioavailability and plasma half-life of Omeprazole are increased in patients with impaired hepatic function, a daily dose of 10-20 mg may be sufficient.
Overdosage
Symptoms and Treatment for Overose, and Antidote(s): None has been reported; Single oral doses of up to 160 mg and total oral doses of up to 300 mg/ day have been given without adverse effects.
Symptoms/Clinical Effects of overdose: The following effects have been selected on the basis of their potential clinical significance: Blurred vision; confusion; diaphoresis (increased sweating); drowsiness; dryness of mouth; flushing; headache; nausea; tachycardia (fast or irregular heartbeat).
Treatment: Since there is no specific antidote for overdose with omeprazole, treatment should be symptomatic and supportive. Due to extensive protein binding, omeprazole is not readily dialyzable. Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation.
Contraindications
There are no known contraindications to the use of Omilock Capsule.
Risk-benefit should be considered when the following medical problem exist: Sensitivity to Omeprazole.
Special Precautions
When gastric ulcer is suspected, the possibility of malignancy should be excluded before treatment with Omilock is instituted, as treatment may alleviate symptoms and delay diagnosis.
Risk-benefit should be considered when the following medical problems exist: Hepatic disease, chronic, current or history of (dosage reduction may be required due to increased half-life in chronic hepatic disease).
High risk groups: Fertility: In a rat fertility and general reproductive performance test, omeprazole, in a dose 35 to 345 times the human dose, was not toxic or deleterious to the reproductive performance of parental animals.
Use in Pregnancy: Adequate and well-controlled studies in humans have not been done and the drug is not recommended.
Studies in pregnant rats did not show omeprazole to have any teratogenic potential at doses 345 times the human dose. Omeprazole produced dose-related increases in embryo-lethality, fetal resorptions, and pregnancy disruptions in rabbits receiving 17 to 172 times the human dose.
In rats, dose-related embryo/fetal toxicity and postnatal developmental toxicity were observed in offspring resulting from parents treated with 35 to 345 times the human dose.
FDA Pregnancy Category C.
Use in Lactation: It is not known whether omeprazole is distributed into human breast milk. However, because omeprazole has been shown to cause tumorigenic and carcinogenic effects in animals, a decision should be made on whether nursing should be discontinued or the medication withdrawn, taking into account the importance of the omeprazole to the mother.
Neonates: There are no data and the drug is not recommended for neonates.
Use in Children: Appropriate studies on the relationship of age to the effects of omeprazole have not been performed in the pediatric population and the drug is not recommended.
Use in Elderly: No information is available on the relationship of age to the effects of omeprazole in geriatric patients. However, a somewhat decreased rate of elimination and an increased bioavailability are more likely to occur in geriatric patients taking omeprazole.
Regular Surveillance: Patients on proton pump inhibitor treatment (particularly those treated for long term) should be kept under regular surveillance.
Subacute Cutaneous Lupus Erythematosus (SCLE): Proton pump inhibitors are associated with very infrequent cases of subacute cutaneous lupus erythematosus (SCLE). If lesions occur, especially in sun-exposed areas of the skin, and if accompanied by arthralgia, the patient should seek medical help promptly and the health care professional should consider stopping omilock. SCLE after previous treatment with a proton pump inhibitor may increase the risk of SCLE with other proton pump inhibitors.
Hypomagnesaemia: Severe hypomagnesaemia has been reported in patients treated with PPI like omilock for at least three months, and in most cases for a year. Serious manifestations of hypomagnesaemia such as fatigue, tetany, delirium, convulsion, dizziness and ventricular arrhythmia can occur but they may begin insidiously and be overlooked.
In most affected patients, hypomagnesaemia improved after magnesium replacement and discontinuation of the PPI.
For patients expected to be on prolonged treatment or who take PPI with digoxin or drugs that may cause hypomagnesaemia (e.g.,diuretics), health care professionals should consider measuring magnesium levels before starting PPI treatment and periodically during treatment.
Fracture: Proton pump inhibitors, especially if used in high doses and over long duration (>1 year) may modestly increase the risk of hip, wrist and spine fracture, predominantly in the elderly or in presence of other recognized risk factors. Observational studies suggest that proton pump inhibitors may increase the overall risk of fracture by 10-40%. Some of this increase may be due to other risk factors. Patients at risk of osteoporosis should receive care according to current clinical guidelines and they should have an adequate intake of vitamin D and calcium.
Clostridium Difficile Diarrhea: Published observational studies suggest that PPI therapy may be associated with an increased of Clostridium difficile associated diarrhea, especially in hospitalized patients. This diagnosis should be considered for diarrhea that does not improve. Patients should use the lowest dose and shortest duration of PPI therapy appropriate to the condition being treated.
Vitamin B12 Deficiency: Daily treatment with any acid-suppressing medications over a long period of time (e.g.,longer than 3 years) may lead to malabsorption of cyanocobalamin deficiency occurring with -suppressing therapy have been reported in the literature. This diagnosis should be considered if clinical symptoms consistent with cyanocobalamin deficiency are observed.
Use In Pregnancy & Lactation
Pregnancy: Adequate and well-controlled studies in humans have not been done and the drug is not recommended.
Studies in pregnant rats did not show omeprazole to have any teratogenic potential at doses 345 times the human dose. Omeprazole produced dose-related increases in embryo-lethality, fetal resorptions, and pregnancy disruptions in rabbits receiving 17 to 172 times the human dose.
In rats, dose-related embryo/fetal toxicity and postnatal developmental toxicity were observed in offspring resulting from parents treated with 35 to 345 times the human dose.
FDA Pregnancy Category C.
Breast-feeding: It is not known whether omeprazole is distributed into human breast milk. However, because omeprazole has been shown to cause tumorigenic and carcinogenic effects in animals, a decision should be made on whether nursing should be discontinued or the medication withdrawn, taking into account the importance of the omeprazole to the mother.
Adverse Reactions
Omeprazole capsule is well tolerated and adverse reactions have generally been mild and reversible. The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate) - not necessarily inclusive:Those indicating need for medical attention: Incidence rare: Hematologic abnormalities, specifically anemia (unusual tiredness of weakness); eosinopenia; leukocytosis (sore throat and fever); neutropenia (continuing ulcers or sores in mouth); pancytopenia or thrombocytopenia (unusual bleeding or bruising); hematuria (bloody urine); proteinuria (cloudy urine); urinary tract infection (bloody or cloudy urine; difficult, burning, or painful urination; frequent urge to urinate).
Those indicating need for medical attention only if they continue or are bothersome: Incidence more frequent: Abdominal pain or colic.
Incidence less frequent: Asthenia (muscle pain; unusual tiredness); central nervous system (CNS) disturbances, specifically dizziness, headache, somnolence (unusual drowsiness); or unusual tiredness; chest pain; gastrointestinal disturbances, specifically acid regurgitation (heartburn); constipation; diarrhea or loose stools; flatulence (gas); or nausea and vomiting; skin rash or itching, urticaria and pruritus, paresthesia, insomnia and vertigo. Blurred vision, taste disturbance, peripheral oedema, increased sweating, gynaecomastia, bronchospasm, encephalopathy in patients with preexisting severe liver disease, hepatitis with or without jaundice, rarely interstitial nephritis and hepatic failure.
Increase in liver enzymes have been observed.
Subactute Cutaneous Lupus Erythematosus (SCLE): Skin and subcutaneous tissue disorders: Frequency not known: Subcutaneous lupus erythematosus.
Interstitial Nephritis: Renal and urinary disorders: lnterstitial nephritis.
Hypomagnesaemia: Metabolism and nutritional disorders:
Frequency not known: hypomagnesaemia.
Fracture: Musculoskeletal disorders: Frequency uncommon: Fracture of the hip, wrist or spine.
Clostridium Difficile Diarrhea: Infection & infestations: Clostridium difficile associated diarrhea.
Fundic Gland Polyps: Gastrointestinal disorders: Frequency common: Fundic gland polyps (benign).
Vitamin B12 Deficiency: Metabolic/Nutritional: Vitamin B12 deficiency.
Drug Interactions
Digoxin: Simultaneous treatment with omeprazole and digoxin in healthy subjects lead to a 10% increase in the bioavailability of digoxin as a consequence of the increased intragastric pH.
Diazepam, Phenytoin and Warfarin: Omeprazole inhibits the metabolism of drugs metabolised by the hepatic cytochrome P450 enzyme system and may increase plasma concentrations of diazepam, phenytoin, and warfarin.
Aminopyrine and Antipyrine: Administration of 60 mg daily for 2 weeks caused a 10-20% prolongation of aminopyrine and antipyrine half-life while half this dose had no significant effect. In most animal models, the effects of omeprazole on barbiturate sleeping times and antipyrine clearance are less marked than those caused by cimetidine.
Theophylline, Propranolol and 7 ethoxycoumarin de-ethylase: Omeprazole does not interfere with theophylline or propranolol metabolism. In one study, however, omeprazole was a more potent inhibitor of 7 ethoxycoumarin de-ethylase activity than cimetidine.
Metoprolol, Lidocaine, Quinidine, Amoxycillin or Antacids: There is no evidence of interaction with theophylline, propranolol, metoprolol, lidocaine, quinidine, amoxycillin or antacids, but interaction with other drugs also metabolised via cytochrome P-450 system cannot be excluded.
Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.
Ampicillin esters, Iron salts or Ketoconazole: Omeprazole may increase gastrointestinal pH; concurrent use with omeprazole may result in a reduction in absorption of ampicillin esters, iron salts, or ketoconazole.
Bone marrow depressants: Concurrent use of omeprazole with these medications may increase the leukopenic and/or thrombocytopenic effects of both these medications; if concurrent use is required, close observations for toxic effects should be considered.
Storage
Store in a dry place, below 30°C, in a tight container. Protect from light.
Shelf-Life: 3 years.
ATC Classification
A02BC01 - omeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Presentation/Packing
Cap 20 mg (caramel/pink coloured hard gelatin, size"2", containing off-white granules) x 2 x 7's.
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